Author/Authors :
Amy J. Pfizenmayer، نويسنده , , Matthew D. Vera، نويسنده , , Xiaobin Ding، نويسنده , , Dong Xiao، نويسنده , , Wei-Chuan Chen، نويسنده , , Madeleine M. Joullié، نويسنده , , Deepika Tandon، نويسنده , , Peter L. Toogood، نويسنده ,
Abstract :
A didemnin B analog containing a Tic (1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid) as a conformationally restrained replacement for tyrosine has been synthesized and shown to have comparable potency as a protein biosynthesis inhibitor. Synthetic highlights include an oxidation of an alcohol to an acid in the presence of the sensitive Tic heterocycle and a modified Schmidt-type one-pot macrocyclization.